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Molecules 2017, 22(12), 2269; doi:10.3390/molecules22122269

Vanadium Compounds as PTP Inhibitors

Developmental Biology and Cancer Programme, UCL Great Ormond Street Institute of Child Health, 30 Guilford Street, London WC1N 1EH, UK
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Received: 30 November 2017 / Revised: 14 December 2017 / Accepted: 15 December 2017 / Published: 19 December 2017
(This article belongs to the Special Issue Protein-Tyrosine Phosphatase Inhibitors)
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Abstract

Phosphotyrosine signaling is regulated by the opposing actions of protein tyrosine kinases (PTKs) and protein tyrosine phosphatases (PTPs). Here we discuss the potential of vanadium derivatives as PTP enzyme inhibitors and metallotherapeutics. We describe how vanadate in the V oxidized state is thought to inhibit PTPs, thus acting as a pan-inhibitor of this enzyme superfamily. We discuss recent developments in the biological and biochemical actions of more complex vanadium derivatives, including decavanadate and in particular the growing number of oxidovanadium compounds with organic ligands. Pre-clinical studies involving these compounds are discussed in the anti-diabetic and anti-cancer contexts. Although in many cases PTP inhibition has been implicated, it is also clear that many such compounds have further biochemical effects in cells. There also remain concerns surrounding off-target toxicities and long-term use of vanadium compounds in vivo in humans, hindering their progress through clinical trials. Despite these current misgivings, interest in these chemicals continues and many believe they could still have therapeutic potential. If so, we argue that this field would benefit from greater focus on improving the delivery and tissue targeting of vanadium compounds in order to minimize off-target toxicities. This may then harness their full therapeutic potential. View Full-Text
Keywords: protein tyrosine phosphatases; PTP; vanadium; oxidovanadium; oxovanadium; vanadate; BMOV; diabetes; cancer protein tyrosine phosphatases; PTP; vanadium; oxidovanadium; oxovanadium; vanadate; BMOV; diabetes; cancer
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Irving, E.; Stoker, A.W. Vanadium Compounds as PTP Inhibitors. Molecules 2017, 22, 2269.

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